GSK3787
Based on 17 publication(s) in Google Scholar
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 188591-46-0
- Fòrmula: C15H12ClF3N2O3S
- Peso molecular:392.78
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GSK3787
More- Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]
- Cell Death Dis. 2025 May 9;16(1):371. [Abstract]
- Biol Psychiatry. 2021 Mar 15;89(6):615-626. [Abstract]
- Food Res Int. 2024 Jan:175:113783. [Abstract]
- Int J Biol Macromol. 2026 Feb:347:150740. [Abstract]
- Cell Rep. 2023 Oct 3;42(10):113211. [Abstract]
- Environ Pollut. 2024 Feb 15:343:123167. [Abstract]
- J Ethnopharmacol. 2025 Sep 6;355(Pt A):120571. [Abstract]
- Biomolecules. 2025 Mar 27;15(4):492. [Abstract]
- Front Pharmacol. 2018 Jun 28:9:648. [Abstract]
- Toxics. 2024 Mar 14;12(3):214. [Abstract]
- Cell Signal. 2020 Aug;72:109628. [Abstract]
- Oncol Res. 2019 Aug 8;27(8):923-933. [Abstract]
- iScience. 2021 Sep 25;24(10):103170. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2020 Dec 29;52(12):1373-1381. [Abstract]
- Nutrition. 2019 Apr:60:217-226. [Abstract]
- Sci Total Environ. 2024 Feb 20:912:168949. [Abstract]
Customer Validation & Images
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WB
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RT-PCR
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RT-PCR
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IHC
Actividad biológica
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PPARδ 6.6 nM (pIC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-1 | IC50 |
5 μM
Compound: 9, GSK3787
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Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
Antagonist activity against pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as inhibition of GW501516-induced receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
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[PMID: 25768705] |
GSK3787 is identified as a potent and selective hPPARδ ligand (pIC50=6.6) with no measurable affinity for hPPARα or hPPARγ (pIC50 < 5) in our standard in vitro ligand displacement assay. GSK3787 is inactive against hPPARα and hPPARγ in similar functional antagonist assays. GSK3787 fails to activate the receptor in a standard hPPARδ-GAL4 chimera cell-based reporter assay. GSK3787 is a selective PPARδ antagonist with equipotent species activity against the human and mouse receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 188591-46-0
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Appearance Solid
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Peso molecular 392.78
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Fòrmula C15H12ClF3N2O3S
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Color White to off-white
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SMILES
O=C(NCCS(=O)(C1=NC=C(C(F)(F)F)C=C1)=O)C2=CC=C(Cl)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]2020 Apr 14;11(1):1792. PMID: 32286289 -
Cell Death Dis
CILP1 interacting with YBX1 promotes hypertrophic scar formation by suppressing PPARs transcription. [Abstract]2025 May 9;16(1):371. PMID: 40346063 -
Biol Psychiatry
Transcription Factor TWIST1 Integrates Dendritic Remodeling and Chronic Stress to Promote Depressive-like Behaviors. [Abstract]2021 Mar 15;89(6):615-626. PMID: 33190845 -
Food Res Int
Fisetin, a dietary flavonoid, promotes transintestinal cholesterol excretion through the activation of PPARδ. [Abstract]2024 Jan:175:113783. PMID: 38129008 -
Int J Biol Macromol
Visceral obesity-induced METTL27 regulation of the FABP5/PPARD/CPT1A axis in promoting colorectal cancer progression. [Abstract]2026 Feb:347:150740. PMID: 41651272 -
Cell Rep
Lipid accumulation-mediated histone hypoacetylation drives persistent NK cell dysfunction in anti-tumor immunity. [Abstract]2023 Oct 3;42(10):113211. PMID: 37792534 -
Environ Pollut
Perturbation of IP3R-dependent endoplasmic reticulum calcium homeostasis by PPARδ-activated metabolic stress leads to mouse spermatocyte apoptosis: A direct mechanism for perfluorooctane sulfonic acid-induced spermatogenic disorders. [Abstract]2024 Feb 15:343:123167. PMID: 38110051 -
J Ethnopharmacol
Chrysanthemum morifolium Ramat. water extract prevents and treats metabolic-associated fatty liver disease via pan-PPAR activity. [Abstract]2025 Sep 6;355(Pt A):120571. PMID: 40921229 -
Biomolecules
PPARs Activity Affects the Hatchability Through Lipid Metabolism Regulation in Silkworm, Bombyx mori L. [Abstract]2025 Mar 27;15(4):492. PMID: 40305260 -
Front Pharmacol
PPARβ/δ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells by Promoting Apoptosis. [Abstract]2018 Jun 28:9:648. PMID: 30002625 -
Toxics
Differential Disruption of Glucose and Lipid Metabolism Induced by Phthalates in Human Hepatocytes and White Adipocytes. [Abstract]2024 Mar 14;12(3):214. PMID: 38535947 -
Cell Signal
CD137 signaling induces macrophage M2 polarization in atherosclerosis through STAT6/PPARδ pathway. [Abstract]2020 Aug;72:109628. PMID: 32247042 -
Oncol Res
PPARβ/δ Agonist GW501516 Inhibits Tumorigenesis and Promotes Apoptosis of the Undifferentiated Nasopharyngeal Carcinoma C666-1 Cells by Regulating miR-206. [Abstract]2019 Aug 8;27(8):923-933. PMID: 30982495 -
iScience
2021 Sep 25;24(10):103170. PMID: 34646996 -
Acta Biochim Biophys Sin (Shanghai)
AT1-receptor autoantibody exposure in utero contributes to cardiac dysfunction and increased glycolysis in fetal mice. [Abstract]2020 Dec 29;52(12):1373-1381. PMID: 33231607 -
Nutrition
β-hydroxy-β-methylbutyrate (HMB) improves mitochondrial function in myocytes through pathways involving PPARβ/δ and CDK4. [Abstract]2019 Apr:60:217-226. PMID: 30677545
GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]
Leu and HMB stimulate the protein expression of PPARβ/δ and CDK4, and GSK3787 and LY2835219 block the protein expression of PPARβ/δ and CDK4.
GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]
The mRNA expression levels of AMPKα, Sirt1, PGC-1α change significantly with the treatment of GSK3787 or LY2835219 are showed.
GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]
The mRNA expression levels of Nrf-1, TFAM, MEF-2A, MEF-2CD, and MEF-2C change significantly with the treatment of GSK3787 or LY2835219 are showed.
GSK3787 purchased from MedChemExpress. Usage Cited in: Nutrition. 2019 Apr:60:217-226. [Abstract]
GSK3787 significantly reverse the beneficial effects of Leu and HMB on mitochondrial mass.
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Sci Total Environ
PPARβ/δ-ANGPTL4 axis mediates the promotion of mono-2-ethylhexyl phthalic acid on MYCN-amplified neuroblastoma development. [Abstract]2024 Feb 20:912:168949. PMID: 38042186
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (127.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.36 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Mice[2]
For RNA and DNA analysis, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or GW0742 and GSK3787 by oral gavage 3 h before euthanasia. After euthanasia, colons are carefully dissected. To isolate colon epithelium, colons are flushed with phosphate-buffered saline, and epithelial cells are scraped from mucosa using a razor blade. The isolated tissues are used for RNA isolation. For glucose-tolerance tests, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or Rosiglitazone (20 mg/kg) by oral gavage once a day for 2 weeks.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (289 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shearer BG, et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010 Feb 25;53(4):1857-61. [Content Brief]
[2]. Palkar PS, et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010 Sep;78(3):419-30. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5460 mL | 12.7298 mL | 25.4595 mL | 63.6489 mL |
| 5 mM | 0.5092 mL | 2.5460 mL | 5.0919 mL | 12.7298 mL | |
| 10 mM | 0.2546 mL | 1.2730 mL | 2.5460 mL | 6.3649 mL | |
| 15 mM | 0.1697 mL | 0.8487 mL | 1.6973 mL | 4.2433 mL | |
| 20 mM | 0.1273 mL | 0.6365 mL | 1.2730 mL | 3.1824 mL | |
| 25 mM | 0.1018 mL | 0.5092 mL | 1.0184 mL | 2.5460 mL | |
| 30 mM | 0.0849 mL | 0.4243 mL | 0.8487 mL | 2.1216 mL | |
| 40 mM | 0.0636 mL | 0.3182 mL | 0.6365 mL | 1.5912 mL | |
| 50 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2730 mL | |
| 60 mM | 0.0424 mL | 0.2122 mL | 0.4243 mL | 1.0608 mL | |
| 80 mM | 0.0318 mL | 0.1591 mL | 0.3182 mL | 0.7956 mL | |
| 100 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6365 mL |
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